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European Journal of Drug Metabolism and Pharmacokinetics

Aiko Iida, Shohei Ouchi, Toshio Oda, Jun Aketagawa, Yasuhiko Ito, Yusuke Takizawa, Mikio Tomita, Masahiro Hayashi
The Editor-in-Chief has retracted this article [1] based on an investigation by the Ministry of Education, Culture, Sports, Science and Technology, Japan, which found that the article contained overlap with a previously published article by Kalitsky-Szirtes J, et al. [2].
November 14, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Slobodan M Janković
BACKGROUND: Individualizing drug dosing regimens in critically ill patients on renal replacement therapy is a challenge to clinicians as guidelines are often imprecise and specific-validated pharmacokinetic software is unavailable. OBJECTIVE: A case of a septic patient on hemodialysis is presented, where a quick solution for antibiotic dose adjustment based on the application of pharmacokinetic principles was found. METHODS: The dose adjustment was made in two steps-the first step was to calculate total antibiotic clearance (using the formula: total drug clearance = dialysate flow rate × fraction of unbound drug in plasma + extrarenal clearance), and the second step was to calculate maintenance dose based on target plasma concentrations in steady-state (using the formula: maintenance dose = target plasma concentration × total drug clearance × dose interval)...
November 13, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Tadatoshi Tanino, Toru Bando, Yuna Okada, Yukie Nojiri, Kanako Hashimoto, Yukari Ueda, Eiichi Sakurai
BACKGROUND AND OBJECTIVES: Mast cell-mediated allergic diseases are a significant global health problem. Nitric oxide (NO) produced by acute type 1 allergies greatly suppresses hepatic cytochrome P450 (CYP) metabolism. A recent in vitro study demonstrated that repeated FcεRI-mediated activation intrinsically modulates mast cell function. We investigated the effect of ovalbumin (OVA) challenges on CYP activity and NO production under real immune responses. METHODS: After repeated sensitization with OVA once a week, serum nitrate plus nitrite (NOx) and total plasma immunoglobulin E concentrations were measured using commercially available kits...
November 8, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Dario Cattaneo, Cristina Gervasoni
Available antiretroviral drugs have demonstrated effectiveness in both pre-exposure prophylaxis and treatment of HIV infection. However, some concerns still persist regarding these therapies, mainly related to patient adherence, drug toxicity and dosing convenience. Cabotegravir is a potent integrase strand transfer inhibitor with a chemical structure similar to dolutegravir that is under clinical evaluation both as oral and long-acting injectable (LAI) formulations for both the prevention or treatment of HIV infection...
November 1, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Ran Xie, Yang Zhang, Nan Zhao, Shuang Zhou, Xin Wang, Wei Han, Yan Yu, Xia Zhao, Yimin Cui
BACKGROUND AND OBJECTIVES: The recombinant human interleukin-1 receptor antagonist (rhIL-1Ra) GR007 is a candidate drug with the potential to prevent the toxicity induced by chemotherapy agents by blocking the IL-1 signaling pathway. The aim of this study was to assess the pharmacokinetics and safety of GR007 in healthy Chinese subjects. METHODS: Thirty subjects received a single intramuscular injection of 30 mg (n = 10), 90 mg (n = 10), or 150 mg (n = 10) GR007...
October 31, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Farnaz Deris Abdolahpour, Lida Abolaliporan Sadegh, Siavoush Dastmalchi, Maryam Hamzeh-Mivehroud, Omid Zarei, Gholamreza Dehgan, Mohammad-Reza Rashidi
BACKGROUND: Aldehyde oxidase (AOX) is an important molybdenum-containing enzyme with high similarity with xanthine oxidase (XO). AOX involved in the metabolism of a large array of aldehydes and N-heterocyclic compounds and its activity is highly substrate-dependent. OBJECTIVES: The aim of this work was to study the effect of five important phenothiazine drugs on AOX activity using benzaldehyde and phenanthridine as aldehyde and N-heterocyclic substrates, respectively...
October 31, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Yan Rong, Patrick Mayo, Mary H H Ensom, Tony K L Kiang
BACKGROUND AND OBJECTIVE: Tacrolimus is the mainstay calcineurin inhibitor frequently administered with mycophenolic acid with or without corticosteroids to prevent graft rejection in adult kidney transplant recipients. The primary objective of this study was to develop and evaluate a population pharmacokinetic model characterizing immediate-release oral tacrolimus co-administered with mycophenolate mofetil (a pro-drug of mycophenolic acid) in adult kidney transplant recipients on corticosteroid-free regimens...
October 30, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Mitsuhiro Nishihara, Hitomi Yamasaki, Richard Czerniak, Helen Jenkins
BACKGROUND AND OBJECTIVES: It was recently proposed that CYP-mediated drug-drug interactions (DDIs) of vonoprazan with clopidogrel and prasugrel can attenuate the antiplatelet actions of the latter two drugs. Clopidogrel is metabolized to the pharmacologically active metabolite H4 and its isomers by multiple CYPs, including CYP2C19 and CYP3A4. Therefore, to investigate the possibility of CYP-based DDIs, in vitro metabolic inhibition studies using CYP probe substrates or radiolabeled clopidogrel and human liver microsomes (HLMs) were conducted in this work...
October 25, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Feng Wu, Xiuli Zhao, Xingang Li, Yimin Cui
BACKGROUND AND OBJECTIVES: The disposition of azithromycin in the human eye following topical administration has not been fully explored. Population pharmacokinetic (PopPK) modeling can allow useful conclusions to be drawn based on limited tear sampling data. The aim of this study was therefore to develop and evaluate a PopPK model of azithromycin eyedrops in tears, investigate typical model parameters, and identify potential covariates following single-dose ocular instillation. METHODS: A total of 84 tear samples were obtained from 42 healthy volunteers at seven time points over 24 h following topical administration of azithromycin eyedrops (2...
October 24, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Ahmad Y Abuhelwa, Stuart Mudge, Richard N Upton, David J R Foster
BACKGROUND AND OBJECTIVE: SUBA-itraconazole and Sporanox are two oral formulations of itraconazole. Drug-drug interactions with omeprazole have been previously reported; however, mechanistic understanding of the pharmacological and physiological interactions of omeprazole with orally administered itraconazole within a population modeling paradigm is lacking. The objective of this analysis was to mechanistically describe and quantify the effect of omeprazole on the pharmacokinetics of itraconazole and its major metabolite, hydroxyitraconazole from the SUBA itraconazole and Sporanox formulations...
October 16, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Antonella Riva, Massimo Ronchi, Giovanna Petrangolini, Stefania Bosisio, Pietro Allegrini
BACKGROUND AND OBJECTIVES: The importance of quercetin and flavonoids in the diet and as food supplements is well known, and literature studies support their potential use to treat several human diseases. Many beneficial properties have been described for quercetin, so much effort has been directed into overcoming the major drawbacks of this natural compound-its poor solubility and low oral absorption. The aims of this study were to compare a new food-grade lecithin-based formulation of quercetin, Quercetin Phytosome® , to unformulated quercetin in terms of solubility in simulated gastrointestinal fluids and oral absorption in a randomized crossover pharmacokinetic study of healthy volunteers...
October 16, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Jennifer Shiu, Grace Ting, Tony Kl Kiang
Delafloxacin has recently received approval by the US Food and Drug Administration for the treatment of acute bacterial skin and skin structure infections. This article provides a balanced and comprehensive systematic critique of the literature in order to provide an up-to-date summary of its clinical pharmacology. Oral delafloxacin is rapidly absorbed and exhibits comparable exposure characteristics (300 mg intravenous versus 450 mg oral) between the two formulations, allowing easy transition from intravenous to oral therapy...
October 15, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Lin-Sen Qing, Ting-Bo Chen, Wen-Xia Sun, Li Chen, Pei Luo, Zhi-Feng Zhang, Li-Sheng Ding
BACKGROUND AND OBJECTIVES: Astragaloside IV (AGS IV) is the most important bioactive constituent of Radix Astragali. However, its disappointing clinical application is mainly caused by its very low solubility in biologic fluids, resulting in poor bioavailability after oral administration. We recently obtained a novel water-soluble derivative of AGS IV (astragalosidic acid, LS-102) that displayed significant cardioprotective potential against hypoxia-induced injury. The objective of this study was to investigate the intestinal absorption, main pharmacokinetic parameters and acute toxicity of LS-102 in rodents compared with AGS IV...
October 12, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Sharoen Yu Ming Lim, Athira Rafhana Binti Azidin, Yee Tze Ung, Mustafa Al-Shagga, Mohammed Abdullah Alshawsh, Zahurin Mohamed, Chin Eng Ong, Yan Pan
BACKGROUND AND OBJECTIVE: A significant number of people worldwide consume khat on daily basis. Long term of khat chewing has shown negative impact on several organ systems. It is likely that these people are co-administered khat preparations and conventional medication, which may lead to khat-drug interactions. This study aimed to reveal the inhibitory potencies of khat ethanol extract (KEE) and its major active ingredient (cathinone) on human cytochrome P450 (CYP) 2C9, CYP2D6, and CYP3A4 enzymes activities, which are collectively responsible for metabolizing 70-80% clinically used drugs...
October 10, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Chandrali Bhattacharya, Danielle Kirby, Michael Van Stipdonk, Robert E Stratford
BACKGROUND AND OBJECTIVES: Bupropion is an atypical antidepressant and smoking cessation aid associated with wide intersubject variability. This study compared the formation kinetics of three phase I metabolites (hydroxybupropion, threohydrobupropion, and erythrohydrobupropion) in human, marmoset, rat, and mouse liver microsomes. The objective was to establish suitability and limitations  for subsequent use of nonclinical species to model bupropion central nervous system (CNS) disposition in humans...
October 8, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Zorica Jović, Slobodan M Janković, Dejana Ružić Zečević, Dragan Milovanović, Srđan Stefanović, Marko Folić, Jasmina Milovanović, Marina Kostić
Second-generation triazoles were developed in response to the quest for more efficacious and safer therapeutic options for the treatment of severe systemic aspergillosis and candidiasis. These agents include voriconazole, posaconazole, isavuconazole, and ravuconazole. The aim of this review was to present and compare the pharmacokinetic characteristics of second-generation triazoles for the treatment of invasive aspergillosis and candidiasis, emphasizing their clinical implications. The MEDLINE, Scopus, EBSCO, Google Scholar, and SCIndeks databases were searched using advanced search options, including the names of second-generation triazoles and pharmacokinetic terms as keywords...
October 3, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Paschoalina Romano, Fabiana Agena, Pérsio de Almeida Rezende Ebner, Nairo Massakazu Sumita, Ana Heloísa Kamada Triboni, Fernanda Ramos, Márcio Dos Santos Garcia, Nilo José Coelho Duarte, Francine Brambate Carvalhinho Lemos, Nelson Zocoler Galante, Elias David-Neto
BACKGROUND AND OBJECTIVES: Elderly patients are increasingly likely to be recipients of transplants. However, the pharmacokinetics of mycophenolic acid (MPA) in this population are yet to be studied in detail. The objective of this study was to assess whether there were differences in MPA pharmacokinetic parameter values between elderly recipients and younger-adult recipients during the 6 months immediately following renal transplantation. METHODS: In this analysis, the longitudinal 12-h pharmacokinetics of MPA, administered as enteric-coated mycophenolate sodium (EC-MPS), were evaluated in 44 elderly renal transplant recipients and compared with the corresponding pharmacokinetics of MPA in 31 younger adult recipients...
September 18, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Jia Hui Wang, Song Hui Hu, Ji Yan Su, Jun Ping Pan, Xiang Nan Mi, Hai Ju Geng, Wei Zhang, Liang Cai, Chao Fen Su, Ai Hua Hong, Huan Min Luo
BACKGROUND AND OBJECTIVES: Methyl 3,4-dihydroxybenzoate (MDHB) has the potential to prevent neurodegenerative diseases (NDDs). The present work aims to reveal the pharmacokinetics and tissue distribution characteristics of MDHB. METHODS: The pharmacokinetics and tissue distribution of MDHB were analyzed using LC-MS/MS after a single intragastric administration (50 to 450 mg/kg) in mice, and samples were collected from five animals at specific time points. RESULTS: Pharmacokinetic parameters of MDHB following intragastric administrations were: the time to peak concentration (Tmax ) ranged from 0...
September 17, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Ting Huang, Yanan Liu, Chengliang Zhang
Baicalin is one of the major bioactive components of Scutellaria radix, a Chinese herb that has been used since ancient times. Baicalin has various pharmacological activities, including antitumor, antimicrobial, and antioxidant, and has wide clinical applications. Baicalin displays a distinct pharmacokinetic profile including gastrointestinal hydrolysis, enterohepatic recycling, carrier-mediated transport, and complicated metabolism. The in vivo disposition of baicalin is affected by combinations of other herbs and baicalin can interact with other co-administered drugs due to competition between metabolic enzymes and protein binding...
September 12, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Renjie Xu, Ying Peng, Mengyue Wang, Xiaobo Li
BACKGROUND: Isoalantolactone and alantolactone are the main sesquiterpene lactones in Radix Inulae (dried root of Inula helenium L. or I. racemosa Hook. F.), which is a frequently utilized herbal medicine. They also occur in several plants and have various pharmacologic effects. However, they have been found to have poor oral bioavailability in rats. OBJECTIVES: To understand the intestinal absorptive characteristics of isoalantolactone and alantolactone as well specific influx and efflux transporters in their absorption...
September 12, 2018: European Journal of Drug Metabolism and Pharmacokinetics
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